Fenbendazole encapsulation method

FIELD: chemistry.

SUBSTANCE: fenbendazole is dissolved in dioxane or dimethyl sulphoxide or dimethyl formamide. The obtained fenbendazole solution is added to a solution of sodium carboxymethyl cellulose in ethyl acetate in the presence of an E472s preparation while stirring at a rate of 1000 rps, wherein the fenbendazole and sodium carboxymethyl cellulose are taken in weight ratio of 1:3. Methyl carbinol and distilled water, taken in volume ratio of 2:1, respectively, are then added. The obtained suspension of microcapsules is filtered and dried. The process of producing fenbendazole microcapsules carried out at 25°C for 20 minutes without special equipment.

EFFECT: improved method.

3 ex

 

The invention relates to the field of encapsulation, in particular the production of microcapsules of fenbendazol.

Previously known methods for producing microcapsules of drugs. Thus, in U.S. Pat. 2092155, IPC A61K 047/02, A61K 009/16 published 10.10.1997, Russian Federation, proposed a method for microencapsulation of drugs, based on the use of irradiation with ultraviolet rays.

The disadvantages of this method are the duration of the process and the use of ultraviolet radiation, which can influence the formation of microcapsules.

In Pat. 2091071, IPC A61K 35/10, Russian Federation, published 27.09.1997, method for obtaining the drug by dispersion in a ball mill to obtain microcapsules.

The disadvantage of this method is the use of a ball mill and the duration of the process.

In Pat. 2101010, IPC A61K 9/52, A61K 9/50, A61K 9/22, A61K 9/20, A61K 31/19, Russian Federation, published 10.01.1998 proposed chewable form of the drug with taste masking, having the properties of a controlled release drug product that contains microcapsules with a size of 100-800 microns in diameter and consists of pharmaceutical kernel crystalline ibuprofen and polymeric coating comprising a plasticizer, elastic enough to resist chewing. Polymer is a coating is a copolymer based on methacrylic acid.

The drawbacks of the invention: use of a copolymer based on methacrylic acid, as these polymer coatings can cause cancer; complexity; the duration of the process.

In Pat. 2173140, IPC A61K 009/50, A61K 009/127, Russian Federation, published 10.09.2001, method for obtaining kremnijorganicheskih microcapsules using a rotary cavitation plants with high shear effort and powerful acoustic phenomena of sound and ultrasound range for dispersion.

The disadvantage of this method is the use of special equipment - rotary-cavity setup, which has the ultrasonic action that affects the formation of microcapsules and can cause adverse reactions due to the fact that ultrasound destructive effect on the polymers of protein nature, therefore the proposed method is applicable when working with polymers of synthetic origin.

In Pat. 2359662, IPC A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published 27.06.2009, Russian Federation, proposed a method of producing microcapsules using spray cooling in the spray tower Niro under the following conditions: air temperature at the inlet 10°C, the temperature at the outlet 28°C, the speed of rotation of the spray drum 10000 Rev/mi is. Microcapsules according to the invention have improved stability and provide adjustable and/or prolonged release of the active ingredient.

Disadvantages of the proposed method are the duration of the process and the use of special equipment, a set of conditions (temperature of inlet air 10°C, the temperature at the outlet 28°C, the speed of rotation of the spray drum 10,000 rpm).

The closest method is the method proposed in U.S. Pat. 2134967 IPC A01N 53/00, A01N 25/28 published 27.08.1999, Russian Federation. Water is dispersed solution of a mixture of natural lipids and a PYRETHROID insecticide in the weight ratio of 2-4:1 in an organic solvent, which leads to simplification of the method of microencapsulation.

The disadvantage of this method is the dispersion in the aquatic environment, which makes the proposed method applicable to the production of microcapsules of water-soluble drugs in water-soluble polymers.

The technical objective is the simplification and acceleration of the process of production of microcapsules, the reduction of losses upon receipt of the microcapsules (increase in mass).

The solution of the technical problem is achieved by the method of encapsulation of fenbendazol in the shell of sodium carboxymethyl cellulose, which consists in the fact that the fenbendazol dissolved in dioxane or dimethyl sulfoxide or Dima is ivoryline, add the resulting solution of fenbendazol to a solution of sodium carboxymethyl cellulose in ethyl acetate in the presence of the drug E472 with under stirring at a speed of 1000 rpm/sec, with fenbendazol and sodium carboxymethyl cellulose charge / mass ratio of 1:3, then add methylcarbamoyl and distilled water taken in a volumetric ratio of 2:1, respectively, obtained suspension of microcapsules are filtered and dried, thus obtaining process microcapsulation carried out at 25°C for 20 min without special equipment.

A distinctive feature of the proposed method is the use of sodium carboxymethyl cellulose as the shell of the microcapsules of fenbendazol as their cores, and the use of two precipitators - methylcarbazole and ethyl acetate.

The result of the proposed method are obtaining microcapsules of fenbendazol in the sodium carboxymethyl cellulose at 25°C for 20 minutes. The output of the microcapsules is over 90%.

EXAMPLE 1. Obtaining microcapsules of fenbendazol with the dissolution of the drug in dioxane, the ratio of the core/polymer 1:3

100 mg of fenbendazol dissolved in 1 ml of dioxane and the resulting mixture was dispersed in a solution of sodium carboxymethyl cellulose in ethyl acetate containing 300 mg of the specified polymer in the presence of 0.01 g of the drug E472 with paramasivan is about 1000/sec. Then poured 2 ml methylcarbazole and 1 ml of distilled water. The resulting suspension is filtered and dried at room temperature.

Received 0,396 g white to yellowish powder. The yield was 99%.

EXAMPLE 2. Obtaining microcapsules of fenbendazol with the dissolution of the drug in dimethyl sulfoxide (DMSO), the ratio of the core/polymer 1:3

100 mg of fenbendazol dissolved in 1 ml DMSO and the mixture was dispersed in a solution of sodium carboxymethyl cellulose in ethyl acetate containing the specified 300 mg of the polymer in the presence of 0.01 g of the drug E472 with when mixing about 1000/sec. Then poured 2 ml methylcarbazole and 1 ml of distilled water. The resulting suspension is filtered and dried at room temperature.

Received 0,396 g white to yellowish powder. The yield was 99%.

EXAMPLE 3. Obtaining microcapsules of fenbendazol with the dissolution of the drug in dimethylformamide (DMF), the ratio of the core/polymer 1:3

100 mg of fenbendazol dissolved in 1 ml DMF and the resulting mixture was dispersed in a solution of sodium carboxymethyl cellulose in ethyl acetate containing the specified 300 mg of the polymer in the presence of 0.01 g of the drug E472 with when mixing about 1000/sec. Then poured 2 ml methylcarbazole and 1 ml of distilled water. The resulting suspension is filtered and dried at room temperature.

Received 0,396 g b the logo with yellowish powder. The yield was 99%.

The obtained microcapsules of fenbendazol physico-chemical method for the deposition nerastvorim using two precipitators - methylcarbazole and ethyl acetate, which increases output and accelerates the process of microencapsulation. The process is simple to perform and lasts for 20 minutes, requires no special equipment.

The proposed method is suitable for the veterinary industry due to the minimal loss of speed, ease of acquisition and allocation of microcapsules.

The method of encapsulation of fenbendazol in the shell of the sodium carboxymethyl cellulose, characterized in that the fenbendazol dissolved in dioxane, or dimethyl sulfoxide, or dimethylformamide, add the resulting solution of fenbendazol to a solution of sodium carboxymethyl cellulose in ethyl acetate in the presence of the drug As under stirring at a speed of 1000 rpm/sec, with fenbendazol and sodium carboxymethylcellulose charge / mass ratio of 1:3, then add methylcarbamoyl and distilled water taken in a volumetric ratio of 2:1, respectively, obtained suspension of microcapsules are filtered and dried, and the process of production of microcapsules of fenbendazol carried out at 25°C for 20 min without special equipment.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to agriculture. Microcapsules of pesticides are obtained by mixing solution of sodium carboxymethylcellulose in cyclohexanol in presence of a surface-active substance with solution of pesticides in dimethylsulfoxide with further addition of ethanol after formation of solid phase.

EFFECT: invention makes it possible to simplify the process of obtaining microcapsules of preparation in water-soluble polymers, and increase weight output.

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to method of obtaining microcapsules of medication of cephalosporin group in konjac gum. In accordance with claimed method cephalosporin powder, preliminarily dissolved in dimethylformamide, and surface-active substance are added to konjac gum solution in isopropyl alcohol, with addition of carbinol after formation of independent solid phase by cephalosporin. Obtained suspension of microcapsules is filtered, washed with acetone and dried in dessicator.

EFFECT: invention makes it possible to simplify and accelerate process of obtaining microcapsules of water-soluble medications of cephalosporin groups in konjac gum, as well as to increase their output by weight.

4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to method of obtaining microcapsules of medication of cephalosporin group in poludanum. In accordance with claimed method cephalosporin powder and surface-active substance are added to aqueous solution of poludanum, mixture is mixed until components dissolve completely, after formation of transparent solution carbinol and after it isopropyl alcohol are additionally poured in. Obtained suspension of microcapsules is filtered, washed with acetone and dried in dessicator.

EFFECT: invention makes it possible to simplify and accelerate process of obtaining microcapsules of water-soluble medications of cephalosporin groups in poludanum, as well as to increase their output by weight.

4 ex

FIELD: veterinary medicine.

SUBSTANCE: method comprises the use of encapsulated fenbendazol. Sodium carboxymethyl cellulose is used as coating of the microcapsules. The microcapsules are obtained by the physico-chemical method of nonsolvent addition using two precipitators - carbinol and cyclohexanol. The ratio of core/polymer is 1:3. The preparation is given to animals at a dose of 22.5 mg/kg (15 mg/kg as active agent) as a single dose.

EFFECT: method is simple to use and is highly effective in the treatment of cattle with strongylatosis.

1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for preparing drug microcapsules of cephalosporins in konjak gum in dioxane. According to the declared method, a konjak gum solution in dioxane is added with a surfactant that is a cephalosporin powder pre-dissolved in ethanol, and with carbinol after cephalosporin forms an independent solid phase. The prepared microcapsule suspension is filtered, washed in acetone and dried in a drying oven.

EFFECT: invention enables simplifying and accelerating the process of water-soluble drug microcapsules of cephalosporins in konjak gum, as well as increasing a mass yield.

4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, particularly to a method for preparing drug microcapsules of cephalosporin. The method for preparing drug microcapsules of cephalosporin consists in adding a konjak solution in carbon tetrachloride with a surfactant; a powder of cephalosporin is dissolved in water or ethanol and transferred into the konjak solution in carbon tetrachloride; once the antibiotic has formed an independent solid phase, carbinol and distilled water are added drop-by-drop; the prepared suspension of microcapsules is filtered, washed in acetone and dried; the process of microcapsules is carried out in the certain environment.

EFFECT: method provides simplifying and accelerating the process of microcapsules of water-soluble drug preparations.

7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for preparing interferon-coated cephalosporin microcapsules. The declared method is characterized by mixing 1% aqueous solution of human leukocyte α- or β-interferon, cephalosporin powder and preparation E472c as a surfactant. The prepared mixture is stirred until the reaction components are fully dissolved, and after a transparent solution is generated, methanol 1 ml as a first non-solvent and then isopropyl alcohol 5 ml as a second non-solvent are slowly added drop-by-drop, then filtered, washed in acetone and dried.

EFFECT: invention provides preparing the high-yield cephalosporin microcapsules and ensuring the loss reduction.

8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of cephalosporins related to β-lactam antibiotics. A method for preparing cephalosporin microcapsules is implemented by physicochemical non-solvent addition. That involves using two non-solvents that are carbinol and isopropyl alcohol taken in ratio 1:4. The microcapsule yield makes more than 90%.

EFFECT: method for cephalosporin microcapsules provides accelerating the process for preparing and simplifying the method.

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of drug preparations, vitamins, herbicides, flavouring agents and polysaccharides. The microcapsules are prepared by physical-chemical nonsolvent addition with using benzol as a precipitator.

EFFECT: invention provides simplifying and accelerating the process of preparing the microcapsules, reducing losses in preparing the microcapsules (higher weight yield).

48 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of drug preparations of cephalosporins referred to β-lactam antibiotics in konjac gum by physical-chemical precipitation in a non-solvent. Konjac gum is used as a microcapsule membrane. The microcapsules are prepared by physical-chemical precipitation in the non-solvent with using two precipitation agents - carbinol and chloroform. The process of microcapsules is carried out at 25°C with no special equipment required.

EFFECT: method according to the invention provides simplifying and accelerating the process of microcapsules of drug preparations of cephalosporins, and reducing losses (higher weight yield).

4 ex

FIELD: chemistry.

SUBSTANCE: group of inventions relates to a chelate amphiphilic polymer as a carrier, a particle as a carrier containing a self-assembling structure of a chelating amphiphilic polymer (polymersome), contrast agents for CEST MRT, SPECT, PET or Spectral CT, containing said particle, and a method of producing the particle. The chelate amphiphilic polymer is capable of aggregation and contains a hydrophilic block (MA), having a chelating moiety (X) as a terminal group and a hydrophobic block (MB), wherein the polymer has the formula X-[MA]n - [MB]m, (i), where n and m are integers ranging from 3 to 1000000, which represent the number of monomer links forming the corresponding blocks. The hydrophilic block is selected from polyethylene oxide, polymethacrylic acid, polyacrylamide derivatives, polyvinyl alcohol or polyhydroxyethylmethacrylate, hydrophilic polypeptides and sugar derivatives. The hydrophobic block is selected from polybutadiene, polyisoprene and polyethylethylene. The chelating moiety is selected from a group comprising polyphosphates, amino carboxylic acids, 1,3-diketones, hydroxy carboxylic acids, polyamines, amino alcohols, aromatic heterocyclic bases, phenols, amino phenols, oximes, peptides containing proximal chelate functional groups, Schiff bases, tetrapyrroles, sulphur compounds, synthetic macrocyclic compounds, phosphonic acid or a combination of two or more of said compounds.

EFFECT: invention provides chelate amphiphilic polymers which are capable of self-assembling and are suitable for use in vulcanisation methods.

14 cl, 7 dwg, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to pharmaceutics, namely to a pharmaceutical composition (a solid oral dosage form (a tablet or a capsule)) of tyrosine kinase Bcr-Abl inhibitor - imatinib(4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)-pyrimidin-2-ylamino)phenyl]benzamide). The pharmaceutical composition contains 25-45 wt % of imatinib, preferentially imatinib mesylate, more preferentially an α-crystalline form of imatinib mesylate, a binding agent representing povidone, and at least two desintegrant representing low-substituted hydroxypropyl cellulose and sodium carboxymethyl starch.

EFFECT: invention provides the min 80% imatinib release from the tablet for 15 minutes after oral administration and enables extending the range of drugs used for leukaemia.

14 cl, 4 dwg, 3 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of cephalosporins related to β-lactam antibiotics. A method for preparing cephalosporin microcapsules is implemented by physicochemical non-solvent addition. That involves using two non-solvents that are carbinol and isopropyl alcohol taken in ratio 1:4. The microcapsule yield makes more than 90%.

EFFECT: method for cephalosporin microcapsules provides accelerating the process for preparing and simplifying the method.

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of drug preparations, vitamins, herbicides, flavouring agents and polysaccharides. The microcapsules are prepared by physical-chemical nonsolvent addition with using benzol as a precipitator.

EFFECT: invention provides simplifying and accelerating the process of preparing the microcapsules, reducing losses in preparing the microcapsules (higher weight yield).

48 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of drug preparations of cephalosporins referred to β-lactam antibiotics in konjac gum by physical-chemical precipitation in a non-solvent. Konjac gum is used as a microcapsule membrane. The microcapsules are prepared by physical-chemical precipitation in the non-solvent with using two precipitation agents - carbinol and chloroform. The process of microcapsules is carried out at 25°C with no special equipment required.

EFFECT: method according to the invention provides simplifying and accelerating the process of microcapsules of drug preparations of cephalosporins, and reducing losses (higher weight yield).

4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microencapsulation of drugs through the example of rivanol which can be used as an antimicrobial, antifungal topical preparation. A method for preparing microcaplues of rivanol in a water-soluble polymer representing polyvinyl alcohol or polyvinyl pyrrolidone is implemented by physical-chemical precipitation with a solvent wherein a precipitant is acetone. The process is carried out at 25°C with no special equipment required.

EFFECT: method for preparing the microcapsules of rivanol provides simplifying the process of microencapsulation.

13 dwg, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical microcapsulation of cephalosporins related to β-lactam antibiotics. As a microcapsule shell, the method of pharmaceutical microcapsulation of cephalosporins uses konjac gum; the microcapsules are prepared by physical-chemical technology implying the precipitation in a non-solvent using two precipitants - carbinol and diethyl ester in ratio 1:3; the method is conducted at 25°C with no special equipment.

EFFECT: invention provides simplified and accelerated preparation of the water-soluble pharmaceutical microcapsules of cephalosporins in konjac gum, loss reduction in preparing the microcapsules (higher yield-mass).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: declared group of inventions refers to a pharmacological composition for intranasal introduction for cerebral delivery, and a method for preparing said composition. The declared composition comprises a container base formed by porous particles of calcium carbonate and titanium dioxide of particle size 100-5000 nm and a pharmacologically active component - loperamide. The container surface is modified by surfactants specified in polysorbates, or by polymers specified in a group containing glycosaminoglycanes and polypeptides, or their combination. A method for preparing the pharmacological composition consists in preparing the container base by porous particle synthesis, sorption of loperamide in its pore spaces and modification of the container surface by polymers and surfactants by container incubation in their solutions.

EFFECT: invention provides preparing the pharmacological composition which is applicable for cerebral loperamide delivery after the intranasal introduction.

5 cl, 5 dwg, 1 ex

FIELD: medicine.

SUBSTANCE: invention relates to composition for peroral introduction, which possesses properties of modified release. According to invention composition includes pharmaceutically acceptable excipients and complex medication-ion-exchanging resin with coating with modified release, which contains pharmaceutically active medication, combined with pharmaceutically acceptable ion-exchanging resin. Complex has solidified barrier coating with high rupture strength, water-permeable, water-insoluble, which contains polyvinyl acetate polymer, stabiliser and efficient amount of plastifier. Said coating is in fact non-sticky, when applied onto complex in absence of anti-adhesive preparation, if composition presents tablet, complex medication-ion-exchanging resin with coating additionally contains release-retarding substance in matrix together with complex medication-ion-exchanging resin. Invention also relates to product with modified release, including package which contains composition described above.

EFFECT: invention ensures regulated prolonged active agent release without breaking coating integrity, without application of water-soluble impregnating substances and without agglomeration of complex particles during application of coating.

27 cl, 22 ex

FIELD: medicine.

SUBSTANCE: there are described oral dosage forms of risedronate containing safe and effective amount of a pharmaceutical composition containing risedronate, a chelating agent and an agent for effective delayed release of risedronate and the chelating agent in small intestine. The pharmaceutical composition is directly released in a small intestine of a mammal with ensuring pharmaceutically effective absorption of bisphosphonate together with or without food or drinks. Present invention essentially reduces interaction between risedronate and food or drinks which leads to that the active component of bisphosphonate becomes inaccessible to absorption. Thus, the final oral dosage form can be taken with and without food. Further, present invention covers delivery of risedronate and the chelating agent in a small intestine, essentially reducing irritation of upper gastrointestinal tract associated with bisphosphonate therapy. These advantages simplify previous, complicated regimens and can lead to more complete observance of the bisphosphonate therapy regimen.

EFFECT: present invention essentially reduces interaction between risedronate and food or drinks which leads to that the active component of bisphosphonate becomes inaccessible to absorption.

23 cl, 12 ex

FIELD: medicine.

SUBSTANCE: pharmaceutical composition can additionally contain ethylenediaminotetraacetic acid, polyvinyl pyrrolidone, polyvinyl alcohol, a preserving agent specified in a group: Nipagin, Nipasol, benzoic acid, sodium benzoate, sorbic acid, benzalkonium chloride. As a body-forming base, the composition can contain distilled water, polyethylene oxide 400, polyethylene oxide 4000, polyethylene glycol, propylene glycol, a phosphate buffer, a borate buffer, an acetate-borate buffer depending on a dosage form.

EFFECT: high therapeutic effectiveness, prolonged corneal contact of the preparation which reduces the number of instillations, avoids a risk of side effects and provides good tolerance.

5 cl, 5 ex

Up!